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https://www.readbyqxmd.com/read/28102731/microfluidic-whole-blood-testing-of-platelet-response-to-pharmacological-agents
#1
Ruizhi Li, Tilo Grosser, Scott L Diamond
Platelets present a number of intracellular and transmembrane targets subject to pharmacological modulation, either for cardiovascular disease reduction or as an unintended drug response. Microfluidic devices allow human blood to clot on a defined surface under controlled hemodynamic and pharmacological conditions. The potencies of a number of antiplatelet and anticancer drugs have been tested with respect to platelet deposition on collagen under flow. Inhibitors of cyclooxygenase-1 (COX-1) reduce platelet deposition, either when added ex vivo to blood or ingested orally by patients prior to testing...
January 19, 2017: Platelets
https://www.readbyqxmd.com/read/28102586/creatinine-in-urine-a-method-comparison
#2
Marc Luginbühl, Wolfgang Weinmann
Drug screening in urine is widely applied in forensic toxicology. Contrary to blood analysis, excessive or reduced fluid intake can substantially alter the concentration of substances in urine. As a standard to detect urinary dilution, creatinine concentrations are analyzed. A sample with a concentration below 20 mg/dL is generally defined as too diluted to provide a valid result in abstinence control samples. This work investigates the potential of three different methods for the determination of creatinine concentrations in urine samples: A ZIC-HILIC based LC-MS/MS method, a spectrophotometric method on an AU 480 chemistry system, and a portable, immunoassay based point-of-care testing device was compared by measuring 200 urine samples...
January 19, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28101829/autism-spectrum-disorders%C3%A2-diagnosis-and-management
#3
REVIEW
Sharmila Banerjee Mukherjee
Autism Spectrum Disorder (ASD) is a neuro-developmental disorder commonly seen in children. It is characterized by age inappropriate, impaired social communication and the presence of stereotypic behavior. This disorder is hypothesized to result from cerebral dysfunction arising from a complex interaction between genetic, epigenetic and environmental factors. ASD should be suspected in children failing ASD specific screening tests, in the presence of red flags in social, language and/or play domains, in children with developmental or language delay, abnormal behavior, poor school performance or in those who are at high risk...
January 19, 2017: Indian Journal of Pediatrics
https://www.readbyqxmd.com/read/28099856/screening-bioactives-reveals-nanchangmycin-as-a-broad-spectrum-antiviral-active-against-zika-virus
#4
Keiko Rausch, Brent A Hackett, Nathan L Weinbren, Sophia M Reeder, Yoel Sadovsky, Christopher A Hunter, David C Schultz, Carolyn B Coyne, Sara Cherry
Zika virus is an emerging arthropod-borne flavivirus for which there are no vaccines or specific therapeutics. We screened a library of 2,000 bioactive compounds for their ability to block Zika virus infection in three distinct cell types with two different strains of Zika virus. Using a microscopy-based assay, we validated 38 drugs that inhibited Zika virus infection, including FDA-approved nucleoside analogs. Cells expressing high levels of the attachment factor AXL can be protected from infection with receptor tyrosine kinase inhibitors, while placental-derived cells that lack AXL expression are insensitive to this inhibition...
January 17, 2017: Cell Reports
https://www.readbyqxmd.com/read/28096850/expression-analysis-of-multiple-genes-may-involve-in-antimony-resistance-among-leishmania-major-clinical-isolates-from-fars-province-central-iran
#5
Nafiseh Ghobakhloo, Mohammad Hossein Motazedian, Majid Fardaei
BACKGROUND: Treatment of Cutaneous Leishmaniasis (CL) is being faced with serious difficulties in Fars Province, due to emerging of resistance against meglumine antimonite (Glucantime®). In this context, determining some biomarkers for drug sensitivity monitoring seems to be highly essential. Different studies have been carried out to decipher the genes might be involved in antimony resistant phenotype in Leishmania spp. Here, we selected three genes: AQP (as drug transporter), TDR-1-1(as drug activator), and γ-GCS (inducing reduction environment) for comparative expression analysis on clinical resistant and sensitive isolates of L...
April 2016: Iranian Journal of Parasitology
https://www.readbyqxmd.com/read/28095903/identification-and-application-of-anti-inflammatory-compounds-screening-system-based-on-raw264-7-cells-stably-expressing-nf-%C3%AE%C2%BAb-dependent-seap-reporter-gene
#6
Yue Li, Xiaomeng Wang, Juan Ren, Xi Lan, Jing Li, Jing Yi, Li Liu, Yan Han, Sanqi Zhang, Dongmin Li, Shemin Lu
BACKGROUND: NF-κB is one of the key transcription factors in the inflammatory response, transactivates a series of pro-inflammatory genes and is therefore regarded as an important target for anti-inflammatory drug screening. METHOD: We recombined the reporter gene vector with inserting the "neo" transcript into the vector pNF-κB-SEAP, made the reporter gene vector stable in a eukaryotic cell line. The recombinant reporter gene vector we named pNF-κB-SEAP-Neo was transfected into RAW264...
January 18, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28095900/post-stroke-dementia-a-comprehensive-review
#7
REVIEW
Milija D Mijajlović, Aleksandra Pavlović, Michael Brainin, Wolf-Dieter Heiss, Terence J Quinn, Hege B Ihle-Hansen, Dirk M Hermann, Einor Ben Assayag, Edo Richard, Alexander Thiel, Efrat Kliper, Yong-Il Shin, Yun-Hee Kim, SeongHye Choi, San Jung, Yeong-Bae Lee, Osman Sinanović, Deborah A Levine, Ilana Schlesinger, Gillian Mead, Vuk Milošević, Didier Leys, Guri Hagberg, Marie Helene Ursin, Yvonne Teuschl, Semyon Prokopenko, Elena Mozheyko, Anna Bezdenezhnykh, Karl Matz, Vuk Aleksić, DafinFior Muresanu, Amos D Korczyn, Natan M Bornstein
Post-stroke dementia (PSD) or post-stroke cognitive impairment (PSCI) may affect up to one third of stroke survivors. Various definitions of PSCI and PSD have been described. We propose PSD as a label for any dementia following stroke in temporal relation. Various tools are available to screen and assess cognition, with few PSD-specific instruments. Choice will depend on purpose of assessment, with differing instruments needed for brief screening (e.g., Montreal Cognitive Assessment) or diagnostic formulation (e...
January 18, 2017: BMC Medicine
https://www.readbyqxmd.com/read/28095171/drug-interaction-database-sensitivity-with-oral-antineoplastics-an-exploratory-analysis
#8
John B Bossaer, Christan M Thomas
PURPOSE: Drug interactions are a concern in oncology with the shift toward oral antineoplastics (OAs). Using electronic databases to screen for drug interactions with OAs is a common practice. There is little literature to guide clinicians on the reliability of these systems with OAs. The primary objective of this study was to explore the sensitivity of commonly available drug interaction databases in detecting drug interactions with OAs. METHODS: A list of 20 drug interactions with OAs was developed by two Board-certified oncology pharmacists...
January 17, 2017: Journal of Oncology Practice
https://www.readbyqxmd.com/read/28094550/pharmacophore-modelling-atom-based-3d-qsar-generation-and-virtual-screening-of-molecules-projected-for-mpges-1-inhibitory-activity
#9
S Misra, M Saini, H Ojha, D Sharma, K Sharma
COX-2 inhibitors exhibit anticancer effects in various cancer models but due to the adverse side effects associated with these inhibitors, targeting molecules downstream of COX-2 (such as mPGES-1) has been suggested. Even after calls for mPGES-1 inhibitor design, to date there are only a few published inhibitors targeting the enzyme and displaying anticancer activity. In the present study, we have deployed both ligand and structure-based drug design approaches to hunt novel drug-like candidates as mPGES-1 inhibitors...
January 17, 2017: SAR and QSAR in Environmental Research
https://www.readbyqxmd.com/read/28093634/international-osteoporosis-foundation-and-european-calcified-tissue-society-working-group-recommendations-for-the-screening-of-adherence-to-oral-bisphosphonates
#10
A Diez-Perez, K E Naylor, B Abrahamsen, D Agnusdei, M L Brandi, C Cooper, E Dennison, E F Eriksen, D T Gold, N Guañabens, P Hadji, M Hiligsmann, R Horne, R Josse, J A Kanis, B Obermayer-Pietsch, D Prieto-Alhambra, J-Y Reginster, R Rizzoli, S Silverman, M C Zillikens, R Eastell
: Adherence to oral bisphosphonates is low. A screening strategy is proposed based on the response of biochemical markers of bone turnover after 3 months of therapy. If no change is observed, the clinician should reassess the adherence to the treatment and also other potential issues with the drug. INTRODUCTION: Low adherence to oral bisphosphonates is a common problem that jeopardizes the efficacy of treatment of osteoporosis. No clear screening strategy for the assessment of compliance is widely accepted in these patients...
January 16, 2017: Osteoporosis International
https://www.readbyqxmd.com/read/28093274/a-direct-quantitative-pcr-based-measurement-of-herpes-simplex-virus-susceptibility-to-antiviral-drugs-and-neutralizing-antibodies
#11
Dezső P Virók, Ildikó Eszik, Tímea Mosolygó, Kamil Önder, Valéria Endrész, Katalin Burián
Herpes simplex viruses (HSV) are common human pathogens that can cause painful but benign manifestations and recurrent complaints, but can also cause significant morbidity and mortality on infection of the eye or brain and with disseminated infection of an immunosuppressed patient or a neonate. HSV growth inhibition measurement by plaque or yield reduction is a key task in the development of novel antiviral compounds but the manual methods are very labour intensive. The sensitive and specific PCR technology could be an effective method for quantitation of HSV DNA related to virus replication; however the currently described PCR approaches have a major limitation, namely the requirement of purification of DNA from the infected cells...
January 13, 2017: Journal of Virological Methods
https://www.readbyqxmd.com/read/28093042/chloramphenicol-stereoisomers-need-to-be-distinguished-consequences-observed-from-a-proficiency-test
#12
Mark Sykes, Tobias Czymai, Thomas Hektor, Matthew Sharman, Michael Knaggs
Although the use of chloramphenicol (CAP) as a veterinary drug is banned in the European Union and many other countries, monitoring for CAP residues in food is routine. Positive detections are few, but taken extremely seriously. European Union laboratories analysing for CAP should validate methods according to European Commission Decision 2002/657/EC, must be accredited to ISO 17025, and will generally participate in proficiency testing (PT) schemes, such as those offered by the Food Analysis Performance Assessment Scheme (FAPAS®)...
January 17, 2017: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/28092392/the-in-silico-identification-of-human-bile-salt-export-pump-abcb11-inhibitors-associated-with-cholestatic-drug-induced-liver-injury
#13
Lili Xi, Jia Yao, Yuhui Wei, Xin'an Wu, Xiaojun Yao, Huanxiang Liu, Shuyan Li
Drug-induced liver injury (DILI) is one of the major causes of drug attrition and failure. Currently, there is increasing evidence that direct inhibition of the human bile salt export pump (BSEP/ABCB11) by drugs and/or metabolites is one of the most important mechanisms of cholestatic DILI. In the present study, we employ two in silico methods, random forest (RF) and the pharmacophore method, to recognize potential BSEP inhibitors that could cause cholestatic DILI, with the aim of mitigating the risk of cholestatic DILI to some extent...
January 16, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28092111/design-and-synthesis-of-5-substituted-benzo-d-1-3-dioxole-derivatives-as-potent-anticonvulsant-agents
#14
Shiyang Dong, Tiantian Wang, Chundi Hu, Xiaodong Chen, Yi Jin, Zengtao Wang
A series of 5-substituted benzo[d][1,3]dioxole derivatives was designed, synthesized, and tested for anticonvulsant activity using the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens. Neurotoxicity was determined by rotarod test. In the preliminary screening, six compounds, 3a, 3c, 3d, and 4d-f, showed promising anticonvulsant activities in the MES model, and compounds 4c and 4d exhibited full protection against seizures at doses of 300 mg/kg in the scPTZ model. Among the synthesized compounds, 3c as the most active compound showed high protection against the MES-induced seizures with an ED50 value of 9...
January 16, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28090431/a-role-for-3d-printing-in-kidney-on-a-chip-platforms
#15
Ryan D Sochol, Navin R Gupta, Joseph V Bonventre
The advancement of "kidney-on-a-chip" platforms - submillimeter-scale fluidic systems designed to recapitulate renal functions in vitro - directly impacts a wide range of biomedical fields, including drug screening, cell and tissue engineering, toxicity testing, and disease modelling. To fabricate kidney-on-a-chip technologies, researchers have primarily adapted traditional micromachining techniques that are rooted in the integrated circuit industry; hence the term, "chip." A significant challenge, however, is that such methods are inherently monolithic, which limits one's ability to accurately recreate the geometric and architectural complexity of the kidney in vivo...
March 2016: Current Transplantation Reports
https://www.readbyqxmd.com/read/28090167/novel-screening-test-sparks-new-ideas-about-old-drugs
#16
(no author information available yet)
No abstract text is available yet for this article.
January 2017: P & T: a Peer-reviewed Journal for Formulary Management
https://www.readbyqxmd.com/read/28089738/evaluation-of-the-diuretic-activity-of-the-aqueous-and-80-methanol-extracts-of-the-root-of-euclea-divinorum-hiern-ebenaceae-in-sprague-dawley-rats
#17
Beharu Woldemedhin, Teshome Nedi, Workineh Shibeshi, Mekonnen Sisay Shiferaw
BACKGROUND: Diuretics are drugs that increase the formation of urine and are important for the treatment of various diseases including hypertension and edema. The root decoction of Euclea divinorum has been used as a diuretic agent in the traditional medicine. Therefore, this study was aimed to evaluate the diuretic activity of the crude extracts of the roots of Euclea divinorum in Sprague Dawley rats. METHODS: The aqueous extract (AE) and 80% methanol extract (80ME) of the plant were prepared using decoction and maceration, respectively...
January 12, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28089347/virtual-screening-and-experimental-validation-identify-novel-modulators-of-nuclear-receptor-rxr%C3%AE-from-drugbank-database
#18
Dan Xu, Lijun Cai, Shangjie Guo, Lei Xie, Meimei Yin, Ziwen Chen, Hu Zhou, Ying Su, Zhiping Zeng, Xiaokun Zhang
Retinoid X receptor alpha (RXRα), an important ligand-dependent transcription factor, plays a critical role in the development of various cancers and metabolic and neurodegenerative diseases. Therefore, RXRα represents one of the most important targets in modern drug discovery. In this study, Drugbank 2.0 with 1280 old drugs were virtually screened by Glide according to the crystal structure of ligand-binding domain (LBP) of RXRα. 15 compounds selected were tested for their binding and transcriptional activity toward RXRα by Biacore and reporter gene assay, respectively...
December 26, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28088086/design-and-synthesis-of-new-raf-kinase-inhibiting-antiproliferative-quinoline-derivatives-part-2-diarylurea-derivatives
#19
Mohammed I El-Gamal, Mohammad Ashrafuddin Khan, Hamadeh Tarazi, Mohammed S Abdel-Maksoud, Mahmoud M Gamal El-Din, Kyung Ho Yoo, Chang-Hyun Oh
This article describes the design, synthesis, and biological screening of a new series of diarylurea derivatives possessing quinoline nucleus. Nine target compounds were selected by the National Cancer Institute (NCI, Bethesda, Maryland, USA) for in vitro antiproliferative screening against a panel of 58 cancer cell lines of nine cancer types. Following one-dose initial screening, compounds 1d-g and 2b were selected for 5-dose screening in order to calculate their IC50 and total growth inhibition (TGI) values against the cell lines...
January 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28088050/pharmacists-knowledge-of-issues-in-pharmacotherapy-of-epilepsy-using-antiepileptic-drugs-a-cross-sectional-study-in-palestinian-pharmacy-practice
#20
Ramzi Shawahna, Ahlam Atrash, Aman Jebril, Areen Khalaf, Eman Shaheen, Hala Tahboosh
OBJECTIVE: Antiepileptic drugs (AEDs) are mainstay in controlling epileptic seizures. As experts in medications, pharmacists should be able to ensure accuracy of dosing regimens, explain adverse effects, and screen for and alert people with epilepsy (PWE) and their physicians to possible drug-drug interactions (DDIs). The aim of this study was to evaluate pharmacists' knowledge of issues in pharmacotherapy of epilepsy using AEDs. METHODS: This was a cross-sectional observational study conducted in the Palestinian pharmacy practice...
January 11, 2017: Epilepsy & Behavior: E&B
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